Synthesizing method for cephalosporin compound
A synthesis method and compound technology, applied in the direction of organic chemistry and the like, can solve problems such as unfavorable large-scale production, complex process operation, unfavorable environmental protection, etc., and achieve the effects of reducing production cost and environmental protection expenditure, saving solvent, and improving product yield.
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[0058] [Example 1] Preparation of compound 7-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid intermediate of formula 3
[0059] Get the acetonitrile complex of 600g boron trifluoride (wherein BF Content is 17%, equivalent to 1.504mol), 45g methylmercaptotetrazolium (0.388mol), 100g 7-aminocephalosporanic acid (0.366mol) are placed in a reaction flask , react at 30° C. for 1 h, and add 100 g of N,N-dimethylacetamide to obtain an intermediate solution of the compound of formula 3.
Example Embodiment
[0060] [Example 2] Preparation of compound 7-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid intermediate of formula 3
[0061] Get the dimethyl carbonate complex of 250g boron trifluoride (wherein BF Content is 40%, equivalent to 1.475mol), 45g methylmercaptotetrazolium (0.388mol), 100g 7-aminocephalosporanic acid (0.366mol) , 400 g of dimethyl carbonate was placed in a reaction flask, reacted at 30° C. for 1 h, and 100 g of N,N-dimethylformamide was added to obtain the intermediate solution of the compound of formula 3.
Example Embodiment
[0062] [Example 3] Preparation of compound 7-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid intermediate of formula 3
[0063] 45g methylmercaptotetrazolium (0.388mol), 100g 7-aminocephalosporanic acid (0.366mol), 400g diethyl ether were placed in a reaction flask, 150g boron trifluoride (gas) (2.214mol) was introduced, and reacted at 30°C for 1h , 100 g of triethylamine was added to obtain the intermediate solution of the compound of formula 3.
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